| Bioactivity | PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Srtucture Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) [1]. |
| Invitro | PROTAC FGFR2 degrader 1 (0-1000 nM; 72 h) 对 KATO III 和 SNU16 的 IC50 均小于 0.17 nM[1]。PROTAC FGFR2 degrader 1 (500 nM; 12 h; WB) 诱导 KATO III 中 FGFR2 降解，对 FGFR2 具有高度选择性，且是 UPS 依赖性的[1]。PROTAC FGFR2 degrader 1 (500，1000 nM; 24 h) 诱导 KATO III 和 SNU16 细胞在 G0/G1 期的细胞周期阻滞。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PROTAC FGFR2 degrader 1 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | PROTAC FGFR2 degrader 1 (10 mg/kg, 20 mg/kg; Intraperitoneal injection) 在皮下异种移植 SNU16 小鼠模型中抑制胃癌细胞生长，降低肿瘤重量[1]。 PROTAC FGFR2 degrader 1在SD大鼠体内的药动学特征[1]Parameters |
| Formula | C46H54N10O7 |
| Molar Mass | 858.98 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhanzhan Feng, et al. Synthesis and identification of a selective FGFR2 degrader with potent |
PROTAC FGFR2 degrader 1
CAS: F: C46H54N10O7 W: 858.98
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is
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